| 货号 | 15604-500mg |
| 描述 | Ranolazine was developed to protect the heart from transient ischemia, as may occur during angina and infarct.1 It has diverse effects at the cellular level, inhibiting late sodium and potassium currents (IC50s = 3.9-16.6 µM for both) and blocking ligand binding to α1, β1, and β2 adrenergic receptors (Kis = 0.5-19.5 µM for all).2,3,4 Ranolazine inhibits fatty acid β-oxidation leading to decreased acetyl CoA, activation of pyruvate dehydrogenase, and increased glucose oxidation.5,6 It also weakly inhibits mitochondrial respiratory complex I.7 |
| 别名 | RS 43285; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Allely, M.C. and Alps, B.J. The effects of the novel anti-anginal compound RS 43285 on myocardial conduction in the anaesthetized dog. British Journal of Pharmacology 93(2), 375-382 (1988). 2.Shryock, J.C. and Belardinelli, L. Inhibition of late sodium current to reduce electrical and mechanical dysfunction of ischaemic myocardium. British Journal of Pharmacology 153(6), 1128-1132 (2008). 3.Verrier, R.L.,Kumar, K.,Nieminen, T., et al. Mechanisms of ranolazine’s dual protection against atrial and ventricular fibrillation. Europace 15(3), 317-324 (2013). 4.Wang, W.Q.,Robertson, C.,Dhalla, A.K., et al. Antitorsadogenic effects of (±)-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine (ranolazine) in anesthetized rabbits. Journal of Pharmacology and Experimental Therapeutics 325(3), 875-881 (2008). 5.Clarke, B.,Wyatt, K.M. and McCormack, J.G. Ranolazine increases active pyruvate dehydrogenase in perfused normoxic rat hearts: Evidence for an indirect mechanism. Journal of Molecular and Cellular Cardiology 28(2), 341-350 (1996). 6.Zacharowski, K.,Blackburn, B. and Thiemermann, C. Ranolazine, a partial fatty acid oxidation inhibitor, reduces myocardial infarct size and cardiac troponin T release in the rat. European Journal of Pharmacology 418(1-2), 105-110 (2001). 7.Wyatt, K.M.,Skene, C.,Veitch, K., et al. The antianginal agent ranolazine is a weak inhibitor of the respiratory complex I, but with greater potency in broken or uncoupled than in coupled mitochondria. Biochemical Pharmacology 50(10), 1599-1606 (1995). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 500.5 |
| 分子式 | C24H33N3O4 • 2HCl |
| CAS号 | 95635-56-6 |
| 稳定性 | ≥ 2 years |
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